Composition for treating allergic and/or vasomotor rhinitis or allergic conjunctivitis by topical or oral administration, contains synergistic combination of non-sedating antihistamine and leukotriene antagonist

• Main Authors: SZELENYI, ISTVAN, ENGEL, JUERGEN, POPPE, HILDEGARD
• Format: Patent
• Language: English; German
• Published: 23.08.2001
• Edition: 7
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Pharmaceutical composition comprises (separately or in combination): (A) a non-sedating antihistamine (or its salt), other than compounds of the loratadine type; (B) a leukotriene antagonist (or its salt) comprising (B1) leukotriene D 4 antagonists, (B2) 5-lipoxygenase inhibitors or (B3) FLAP (5-lipoxygenase activating protein) antagonists; and (C) conventional carriers and/or extenders or auxiliaries. Independent claims are included for the following: (i) the use of a combination of (A)-(C) for the preparation of a medicament for use as above; (ii) a medicament comprising (A)-(C), for use as above; and (iii) the preparation of the medicaments, by mixing and formulating the appropriate components. - ACTIVITY : Antiallergic; antiinflammatory; ophthalmological. In tests for inhibition of ovalbumin-induced nasal mucosal permeability in sensitized rats, the degree of inhibition was 11% using azelastine alone at 0.01 mg/kg i.p., 7% using montelukast alone at 0.1 mg/kg i.p. and 40% using a combination of azelastine at 0.01 mg/kg i.p. and montelukast at 0.1 mg/kg i.p. - MECHANISM OF ACTION : Antihistamine; leukotriene D 4 antagonist; 5-lipoxygenase inhibitor; FLAP (5-lipoxygenase activating protein) antagonist. The invention relates to a pharmaceutical combination to be administered topically or orally of a non-sedative anti-histamine, with the exception of compounds of the loratadine type, and a leukotriene antagonist, selected from a leukotriene D4 antagonist, or a 5-lipoxygenase inhibitor, or a FLAP antagonist and optionally conventional, physiologically harmless supports, extenders and auxiliary agents, for the prophylaxis and treatment of allergic and/or vasomotor rhinitis or allergic conjunctivitis. Es wird eine pharmazeutische Kombination zur topischen oder oralen Verabreichung aus einem nichtsedierenden Antihistaminikum mit Ausnahme von Verbindungen des Loratadintyps in Kombination mit einem Leukotrien-Antagonisten, ausgewählt aus einem Leukotrien D¶4¶-Antagonisten oder 5-Lipoxygenase-Inhibitor oder FLAP-Antagonisten und gegebenenfalls üblichen physiologisch unbedenklichen Trägern, Streckmitteln und Hilfsstoffen für die Prophylaxe und Behandlung von allergischer und/oder vasomotorischer Rhinitis bzw. allergischer Konjunktivitis beschrieben.